A COMPREHENSIVE REVIEW ON PRODRUGS OF BIOACTIVE OF NATURAL ORIGIN

Prodrugs are bio-reversible, inactive drug by products that can convert into a parent drug inside the body. Around 10% of the medications accepted globally can be categorized as prodrugs. Prodrugs are designed to enhance the site-selective delivery of an active drug by modifying the physicochemical and pharmacokinetic properties of pharmacologically potent compounds. Prodrugs are changed and form active drugs inside the body through enzymatic or non-enzymatic reactions. This article describes the potent secondary metabolites from natural sources that are amenable to prodrug design. A fair number of them have issues of bioavailability and metabolism, resulting in less efficacy, and a prodrug strategy is required to improve their efficacy. This has come into the spotlight recently by achieving encouraging results in most cases. Many phytochemicals are not preferred due to their low solubility, decreased bioavailability, and adverse effects, but these problems can be overcome with the formation of prodrugs of such compounds. Several techniques can be used to synthesize these prodrugs, including biotransformation, electrophilic substitution, esterification, biomodulation, covalent conjugation, and complex formation. A detailed study of the problem encountered by the bioactive of natural origin, the process of formation of their prodrugs and the advancements produced due to the generation of such prodrugs are discussed in this review & takes the focus on the foremost utilization of the prodrug approach, comprising the capability to enhance oral absorption & aqueous solubility, enhance lipophilicity, increase active transport, and also attain site-selective application.